MedChemWatch now online

The new edition of MedChemWatch, the monthly newsletter from our partners at EFMC, is now available online. It includes a round-up of the latest news from several European medicinal chemistry Societies

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From beehive to bone cement – a Chemistry World story

Taking inspiration from honey bees, scientists in South Korea have incorporated a compound used in beehives into a new strong biomaterial with sustained antimicrobial properties.

CAPE-loaded PMMA (left) was found to be stronger than gentamycin-loaded (right) PMMA

Bone cements have been used in surgery since the 1940s and work like a grout to fill the gaps between orthopaedic implants and bones. The most commonly used bone cements are made from a synthetic resin called poly (methyl methacrylate), or PMMA, and have recently been loaded with antibiotics, such as gentamycin, in an attempt to reduce healthcare related infections. However, the addition of antibiotics has raised concerns over antibiotic resistance, potential carcinogenic effects and the reduced mechanical strength of PMMA.

To overcome these potentially harmful limitations, a team led by Jeong Ho Chang at the Korea Institute of Ceramic Engineering and Technology, have developed PMMA bone cement loaded with caffeic acid phenethyl ester (CAPE). CAPE is an active component of bee propolis, a resin-like mixture collected by honey bees from various trees and buds and used to fill small gaps in the beehive. CAPE is thought to have antimicrobial, anti-inflammatory, antioxidant and anti-cancer effects and has already been approved for use in foods, drinks and cosmetics by the Food and Drug Administration.

The researchers were not only able to demonstrate that CAPE-loaded PMMA is an effective antimicrobial against Staphylococcus aureus, but it also has much better compressive strength than antibiotic-loaded PMMA. This impressive strength is thought to be due to a higher packing density caused by reinforced chemical bonding between the PMMA and CAPE through homogeneous loading. In contrast, conventional antibiotic-loaded bone cements are not uniformly mixed and have low loading efficiencies, so the compressive strength is similar to native PMMA. This also explains why CAPE–PMMA exhibits more controlled and sustained antimicrobial release compared to bone cement loaded with gentamycin.

Antoni Tomsia, a biomaterials expert specialising in treatments for bone defects and diseases at the Lawrence Berkeley National Laboratory, University of California, US, thinks that the incorporation of natural antimicrobials is a good idea. However, he emphasises that antimicrobial implants must go hand-in-hand with ‘provider hand hygiene, patient decolonisation efforts, or environmental decontamination, plus sterilisation, to prevent infections.’

Initial studies were carried out in rabbits and Chang believes that CAPE-loaded PMMA bone cement could be used for human clinical applications after therapeutic efficacy evaluation. ‘We are trying to discuss and work with a medical orthopaedics doctor and I think we can report the new clinical data in the near future,’ reveals Chang.

Story first appeared in Chemistry World November 2014, written by Thadchajini Retneswaran.

Hye Sun Lee and Jeong Ho Chang’s article entitled ‘Antimicrobial spine-bone cement with caffeic acid phenethyl ester for controlled release formulation and in vivo biological assessments‘ featured on the cover of issue 2 of MedChemComm

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Meet the MedChemComm team – See where and when you can meet us in 2015

A selection of conferences the journal will be attending in 2015.

The MedChemComm team will be attending a number of conferences in 2015 and we would be delighted to meet you there.

We’re also the team behind MedChemComm’s sister journals OBC, Natural Product Reports, and Molecular BioSystems, so we’ll happily discuss your interdisciplinary research work. In fact, many of our authors choose to publish their research across all of these titles.

Spring

National symposium on Chemical Biology 18-19 February 2015, Mysore, India. Meet Deeksha Gupta.

Directing Biosynthesis IV 25 – 27th March 2015, Norwich, UK. Meet Marie Cote.

MedChemComm, 27-30 April 2015, Hyderabad, India. Meet Deeksha Gupta.

Grassmere Heterocyclic meeting 7th – 11th May, 2015, Grassmere, UK. Meet James Anson.

Summer

Royal Society of Chemistry Organic Chemistry Symposium Series 1st – 5th June 2015, Sendai, Tokyo, Kyoto, Japan. Meet Rich Kelly

American Peptide Symposium 20th – 25th June 2015, Orlando, Florida. Meet Rich Kelly.

ISMSC 28th June – 2nd July 2015, Strasbourg, France. Meet Marie Cote.

7th International Conference on Green and Sustainable Chemistry, July 5 – 8th, Tokyo, Japan. Meet Hiromitsu Urakami.

ESOC 2015 12th – 16th July 2015, Lisbon, Portugal. Meet Marie Cote.

RSC Organic Synthesis 20th – 23rd July 2015, Cambridge, UK. Meet James Anson.

9th CCS National Organic Chemistry conference, 31st July to 3rd August 2015, Changchun, China. Meet Guanqun Song.

9th National Chemical Biology conference, August, Tianjin, China. Meet Guanqun Song.

250th ACS National Meeting & Exposition 16th – 20th August 2015, Boston, USA.

25th International Society of Heterocyclic Chemistry Conference (August 23-28) in Santa Barbara, USA. Meet Jennifer Lee.

Autumn

18th RSC/SCI medicinal chemistry conference 13th – 16th September 2015, Cambridge, UK. Meet James Anson.

26th Symposium on Physical Organic Chemistry, 24 – 26th September, Ehime, Japan. Meet Hiromitsu Urakami.

13th International Kyoto Conference on New Aspects of Organic Chemistry , 9th – 13th November, Kyoto, Japan. Meet Hiromitsu Urakami.

Tateshina Conference, 13th – 15th November, Tateshina, Japan. Meet Hiromitsu Urakami.

BMOS-16 15th – 19th November 2015, Buzios, Brazil. Meet Rich Kelly.

Winter

Pacifichem 15th – 20th December 2015, Hawaii, USA. Meet Marie Cote.

Let us know if you are planning on attending any of these meetings, as we would be happy to meet you there!

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Malcolm Campbell Memorial Prize winners 2015

The Biological and Medicinal Chemistry Sector of the Royal Society of Chemistry is proud to announce the winners of the Malcolm Campbell Memorial Prize for 2015. The prize has been awarded to Miles Congreve, Fiona Marshall and Malcolm Weir for the seminal contributions to G-protein-coupled receptor (GPCR) drug discovery made by Heptares Therapeutics Ltd since the company was founded in 2007.

This work has included building the world-renowned StaR© technology platform for X-ray crystallography of GPCRs and the invention of a number of clinical candidates. The winners are particularly commended on their outstanding publication record, and on their willingness to release data into the public domain.

The Malcolm Campbell Memorial prize commemorates Professor Campbell’s outstanding contributions in a broad range of chemistry and their applications to the understanding of bioactivity. The prize is awarded biennially and the 2015 prize will be presented formally to the winning team during the 18th RSC/SCI Medicinal Chemistry Symposium to be held at Churchill College in Cambridge on 13th to 16th September 2015.

The BMCS Committee wishes to express its gratitude for the high-quality entries from both academia and industry for the 2015 award.

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Changes to the Editorial Board

The turn of a new year brings with it several changes for MedChemComm and our Editorial Board.

Some members of the Editorial Board have reached the end of their terms as Editorial Board members and so have retired from their roles.

As of the 1st January 2015, Professor Gerhard Ecker, Dr David Rees, and Dr Uli Stilz have retired from the Editorial Board.

We would like to take this opportunity to thank David, Gerhard and Uli for all of their contributions to the journal over the past several years. Their invaluable input into the journal, since its launch in 2010, has been greatly appreciated.

We are pleased to say all three are keen to continue their support of MedChemComm and have accepted positions on our Advisory Board effective immediately. We look forward to continuing our relationship with them in their new roles.

Prof. Gerhard Ecker

Prof. Gerhard Ecker

Dr David Rees

Dr David Rees

Dr Uli Stilz

Dr Uli Stilz

Some new faces will be joining the team and more details on exactly who these are will be released shortly – so watch this space!

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In the Pipeline articles from Derek Lowe now featured in MedChemComm

The new year brings a host of new features in MedChemComm. The first of these is that we are now featuring articles by medicinal chemist and blogger Derek Lowe. These articles, which give opinion and insight into both the science and business sides of drug discovery, will be selected from those published in his In the Pipeline column in the Royal Society of Chemistry magazine Chemistry World, bringing this content to a new audience.

Take a look at the first article in issue 1 of MedChemComm, and look out for further announcements about new features in MedChemComm through the year.

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8th BMCS PhD Biological and Medicinal Chemistry Symposium

On 12th Decemeber the Biological and Medicinal Chemistry Sector (BMCS) of the Royal Society of Chemistry  held its eighth postgraduate symposium for PhD students and postdoctoral workers researching in biological or medicinal chemistry and related areas. The day consisted of 11 oral presentations (8 student and 3 keynote) and poster session.

This year’s symposium was a great success with around 150 participants attending, with an excellent scientific standard all around.

The BMCS judges  awarded two prizes on the day; one for the best oral presentation and one for the best poster, with the winners recieving £300 and £150 respectively as well as each getting a year’s subscription to MedChemComm.

Congratulations go to:

Oral presentation winner:  Charlotte Sutherell, University of Cambridge for her talk “Bromodomain Inhibitor Development and Testing to Evaluate the Therapeutic Potential of SMARCA4 in SWI/SNF Mutant Cancers”

Poster winner: Niall Igoe, University College London for his poster on “Epigenetic Drug Discovery: Small Molecule Inhibitors of Class IV Bromodomains”

Oral presentation winner Charlotte Sutherell being presented with her award Poster prize winner Niall Igoie being presented with his award
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Quinoxalines with biological activity

A recent publication in MedChemComm from Doaa A. E. Issa et al.reports the synthesis and biological properties of a series of compounds containing the quinoxaline pharmacophore. Their choice of the quinoxaline motif was inspired by the antineoplastic and antimicrobial activity of other compounds containing this group.

Issa et al. synthesised a total of 15 compounds via a key hydrazino intermediate and evaluated 10 candidates at a single high dose for antitumour activity in the National Cancer Institute-60 cell screen. Compounds showing activity were further evaluated in a multi-dose assay. The team went on to assess the in vitro antibacterial activity and antifungal properties.

They found that several compounds in the series display antibacterial activity and one compound possesses both broad spectrum anticancer activity and antimicrobial activity against Pseudomonas aeruginosa.

Two examples of bioactive quinoxalines

Design, synthesis and biological evaluation of novel 1,2,4-triazolo and 1,2,4-triazino[4,3-a]quinoxalines as potential anticancer and antimicrobial agents
Doaa A. E. Issa, Nargues S. Habib and Abeer E. Abdel Wahab
Med. Chem. Commun., 2015, DOI: 10.1039/C4MD00257A

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What are your colleagues reading in MedChemComm?

The articles below are the most read MedChemComm articles in July, August and September 2014.

Conformational analysis of peramivir reveals critical differences between free and enzyme-bound states
Michele R. Richards, Michael G. Brant, Martin J. Boulanger, Christopher W. Cairo and Jeremy E. Wulff 
DOI: 10.1039/C4MD00168K

A critical assessment of modeling safety-related drug attrition
Daniel Muthas, Scott Boyer and Catrin Hasselgren 
DOI: 10.1039/C3MD00072A

Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors
Nitipol Srimongkolpithak, Sandeep Sundriyal, Fengling Li, Masoud Vedadi and Matthew J. Fuchter  
DOI: 10.1039/C4MD00274A

Synthesis of α-brominated phosphonates and their application as phosphate bioisosteres
A. Michael Downey and Christopher W. Cairo  
DOI: 10.1039/C4MD00255E

The synthesis and functional evaluation of a mitochondria-targeted hydrogen sulfide donor, (10-oxo-10-(4-(3-thioxo-3H-1,2-dithiol-5-yl)phenoxy)decyl)triphenylphosphonium bromide (AP39)
Sophie Le Trionnaire, Alexis Perry, Bartosz Szczesny, Csaba Szabo, Paul G. Winyard, Jacqueline L. Whatmore, Mark E. Wood and Matthew Whiteman 
DOI: 10.1039/C3MD00323J

Identification of an inhibitor of the ubiquitin–proteasome system that induces accumulation of polyubiquitinated proteins in the absence of blocking of proteasome function
Caroline Haglund, Chitralekha Mohanty, Mårten Fryknäs, Padraig D’Arcy, Rolf Larsson, Stig Linder and Linda Rickardson 
DOI: 10.1039/C3MD00386H

Affinity-based target identification for bioactive small molecules
Makoto Kawatani and Hiroyuki Osada 
DOI: 10.1039/C3MD00276D

Anaplastic lymphoma kinase (ALK) inhibitors: a review of design and discovery
Wen-Chieh Wang, Hui-Yi Shiao, Chieh-Chien Lee, Ka-Shu Fung and Hsing-Pang Hsieh  
DOI: 10.1039/C4MD00048J

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain
Apirat Chaikuad, Andrew M. Petros, Oleg Fedorov, Jing Xu and Stefan Knapp  
DOI: 10.1039/C4MD00237G

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Take 1…minute for chemistry in health

Can you explain the importance of chemistry to human health in just 1 minute? If you’re an early-career researcher who is up to the challenge, making a 1 minute video could win you £500.

The chemical sciences will be fundamental in helping us meet the healthcare challenges of the future, and we are committed to ensuring that they contribute to their full potential. As part of our work in this area, we are inviting undergraduate and PhD students, post-docs and those starting out their career in industry to produce an original video that demonstrates the importance of chemistry in health.

We are looking for imaginative ways of showcasing how chemistry helps us address healthcare challenges. Your video should be no longer than 1 minute, and you can use any approach you like.

The winner will receive a £500 cash prize, with a £250 prize for second place and £150 prize for third place up for grabs too.

Stuck for inspiration? Last year’s winning video is a good place to start. John Gleeson’s video was selected based on the effective use of language, dynamic style, creativity and its accurate content.

The closing date for entries to be submitted is 30 January 2015. Our judging panel will select the top five videos. We will then publish the shortlisted videos online and open the judging to the public to determine the winner and the runners up.

For more details on how to enter the competition and who is eligible, join us at the Take 1… page.

Good luck!

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